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α-Cyano-4-hydroxycinnamic acid (α-CHCA) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. In the sensitive U251 cells, α-Cyano-4-hydroxycinnamic acid (α-CHCA) is able to inhibit cell proliferation and induce cell death, having a cytotoxic effect; however, in the less sensitive SW1088 cells, α-CHCA only inhibits cell proliferation but did not induce cell death. Transport by MCT1, 2, and 4 is competitively inhibited by α-CHCA whereas transport by MCT3 is insensitive to α-cyano-4-hydroxy-cinnamic acid. Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications.
| Molecular Weight | 189.17 |
| Formula | C10H7NO3 |
| CAS Number | 28166-41-8 |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Monocarboxylate Transporter (MCT) Products |
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| Silicristin
Silychristin is a flavonoid rich in milk thistle fruits, which has antioxidant effects. Silychristin is an effective inhibitor of thyroid hormone transporter MCT8 and can strongly inhibit T3 uptake with IC50 of 110 nM. |
| AZD3965
AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with a binding affinity of 1.6 nM. |
| 7ACC1
7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters. |
| 7ACC2
7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells. IC50 value: 11 nM ([14C]-lactate influx). |
| UK-5099
UK-5099 (PF-1005023) is a potent inhibitor of the mitochondrial pyruvate carrier (MPC), it inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM. UK-5099 is also a cuproptosis inhibitor. |
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